KFU. Card publication. Fluconazole-Pyridoxine Bis-Triazolium Compounds with Potent Activity against Pathogenic Bacteria and Fungi Including Their Biofilm-Embedded Forms

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FLUCONAZOLE-PYRIDOXINE BIS-TRIAZOLIUM COMPOUNDS WITH POTENT ACTIVITY AGAINST PATHOGENIC BACTERIA AND FUNGI INCLUDING THEIR BIOFILM-EMBEDDED FORMS

Form of presentation

Articles in international journals and collections

Year of publication

2017

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Authors, employees of KFU

Aymaletdinov Aleksandr Maazovich, author

Balakin Konstantin Valerevich, author

Bondar Oksana Viktorovna, author

Garipov Marsel Radyikovich, author

Iksanova Alfiya Gabdulakhatovna, author

Kayumov Ayrat Rashitovich, author

Kiyamov Ayrat Gazinurovich, author

Lisovskaya Svetlana Anatolevna, author

Malaneva Albina Gennadevna, author

Nikitina Elena Vladimirovna, author

Pavelev Roman Sergeevich, author

Sabirova Alina Elbrusovna, author

Shtyrlin Yuriy Grigorevich, author

Bibliographic description in the original language

Garipov M.R. Fluconazole-Pyridoxine Bis-Triazolium Compounds with Potent Activity against Pathogenic Bacteria and Fungi Including Their Biofilm-Embedded Forms / M.R. Garipov, R.S. Pavelyev, S.A. Lisovskaya, E.V. Nikitina, A.R. Kayumov, A.E. Sabirova, O.V. Bondar, A.G. Malanyeva, A.M. Aimaletdinov, A.G. Iksanova, K.V. Balakin, Y.G. Shtyrlin // Journal of Chemistry. - 2017. - Art. �4761650.

Annotation

Two novel quaternary ammonium salts, bis-triazolium derivatives of fluconazole and pyridoxine, were synthesized by reaction of fluconazole with pyridoxine-based synthetic intermediates. The leading compound demonstrated pronounced antimycotic and antibacterial in vitro activity, comparable to or exceeding that of the reference antifungal (fluconazole, terbinafine) and antibacterial/antiseptic (miramistin, benzalkonium chloride) agents. In contrast to many antimicrobials, the leading compound was also active against biofilm-embedded staphylococci and Escherichia coli. While no biofilm structure destruction occurred, all compounds were able to diffuse into the matrix and reduce the number of colony-forming units by three orders of magnitude at 16 × MBC. The leading compound was significantly less toxic than miramistin and benzalkonium chloride and more toxic than the reference antifungal drugs. The obtained results make the described chemotype a promising starting point for the developme

Keywords

Pathogenic Bacteria

The name of the journal

Journal of Chemistry

URL

https://www.hindawi.com/journals/jchem/2017/4761650/

Please use this ID to quote from or refer to the card

https://repository.kpfu.ru/eng/?p_id=174101&p_lang=2

Full metadata record

Field DC	Value	Language
dc.contributor.author	Aymaletdinov Aleksandr Maazovich	ru_RU
dc.contributor.author	Balakin Konstantin Valerevich	ru_RU
dc.contributor.author	Bondar Oksana Viktorovna	ru_RU
dc.contributor.author	Garipov Marsel Radyikovich	ru_RU
dc.contributor.author	Iksanova Alfiya Gabdulakhatovna	ru_RU
dc.contributor.author	Kayumov Ayrat Rashitovich	ru_RU
dc.contributor.author	Kiyamov Ayrat Gazinurovich	ru_RU
dc.contributor.author	Lisovskaya Svetlana Anatolevna	ru_RU
dc.contributor.author	Malaneva Albina Gennadevna	ru_RU
dc.contributor.author	Nikitina Elena Vladimirovna	ru_RU
dc.contributor.author	Pavelev Roman Sergeevich	ru_RU
dc.contributor.author	Sabirova Alina Elbrusovna	ru_RU
dc.contributor.author	Shtyrlin Yuriy Grigorevich	ru_RU
dc.date.accessioned	2017-01-01T00:00:00Z	ru_RU
dc.date.available	2017-01-01T00:00:00Z	ru_RU
dc.date.issued	2017	ru_RU
dc.identifier.citation	Garipov M.R. Fluconazole-Pyridoxine Bis-Triazolium Compounds with Potent Activity against Pathogenic Bacteria and Fungi Including Their Biofilm-Embedded Forms / M.R. Garipov, R.S. Pavelyev, S.A. Lisovskaya, E.V. Nikitina, A.R. Kayumov, A.E. Sabirova, O.V. Bondar, A.G. Malanyeva, A.M. Aimaletdinov, A.G. Iksanova, K.V. Balakin, Y.G. Shtyrlin // Journal of Chemistry. - 2017. - Art. �4761650.	ru_RU
dc.identifier.uri	https://repository.kpfu.ru/eng/?p_id=174101&p_lang=2	ru_RU
dc.description.abstract	Journal of Chemistry	ru_RU
dc.description.abstract	Two novel quaternary ammonium salts, bis-triazolium derivatives of fluconazole and pyridoxine, were synthesized by reaction of fluconazole with pyridoxine-based synthetic intermediates. The leading compound demonstrated pronounced antimycotic and antibacterial in vitro activity, comparable to or exceeding that of the reference antifungal (fluconazole, terbinafine) and antibacterial/antiseptic (miramistin, benzalkonium chloride) agents. In contrast to many antimicrobials, the leading compound was also active against biofilm-embedded staphylococci and Escherichia coli. While no biofilm structure destruction occurred, all compounds were able to diffuse into the matrix and reduce the number of colony-forming units by three orders of magnitude at 16 × MBC. The leading compound was significantly less toxic than miramistin and benzalkonium chloride and more toxic than the reference antifungal drugs. The obtained results make the described chemotype a promising starting point for the developme	ru_RU
dc.language.iso	ru	ru_RU
dc.subject		ru_RU
dc.title	Fluconazole-Pyridoxine Bis-Triazolium Compounds with Potent Activity against Pathogenic Bacteria and Fungi Including Their Biofilm-Embedded Forms	ru_RU
dc.type	Articles in international journals and collections	ru_RU